Synthesis of new 1‐(2‐, 3‐, or 4‐methanesulfonylphenyl)‐2‐[5‐(<i>N</i>‐hydroxypyridin‐2(1<i>H</i>)‐one)]acetylene regioisomers: A search for novel cyclooxygenase and lipoxygenase inhibitors
Why this work is in the frame
A frame that forgets how it found something cannot be audited. These are the routes that admitted this work.
Bibliographic record
Abstract
Abstract magnified image A group of acetylene regioisomers were designed such that a cyclooxygenase‐2 (COX‐2) SO 2 Me pharmacophore was located at the ortho‐, meta‐, or para‐position of the acetylene C‐1 phenyl ring, and an iron‐chelating 5‐lipoxygenase (5‐LOX) N ‐hydroxypyridin‐2(1 H )‐one moiety was attached via its C‐5 position to the C‐2 position on an acetylene template (scaffold). These target linear acetylene regioisomers were synthesized via a palladium‐catalyzed Sonogashira cross‐coupling reaction. Structure‐activity data acquired using in vitro cell‐based inhibition assays indicated that this novel class of 1‐(2‐, 3‐, or 4‐methanesulfonylphenyl)‐2‐[5‐( N ‐hydroxypyridin‐2(1 H )‐one)]acetylene regioisomers did not inhibit the COX‐2 or (5‐LOX) enzymes, and that they are devoid of in vivo anti‐inflammatory activities. J. Heterocyclic Chem., 46 , 58 (2009).
Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.
Full frame distilled prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.
Codex and Gemma teacher scores by category
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.001 | 0.001 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.001 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| Insufficient payload (model declined to judge) | 0.000 | 0.000 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it